Collaborations Pharmaceuticals, Inc., 840 Main Campus Drive, Lab 3510, Raleigh, NC, 27606, USA.
Integrated Research Facility, Division of Clinical Research, National Institute of Allergy and Infectious Diseases, National Institutes of Health, Frederick, MD, USA.
Antiviral Res. 2020 Oct;182:104908. doi: 10.1016/j.antiviral.2020.104908. Epub 2020 Aug 13.
We have recently identified three molecules (tilorone, quinacrine and pyronaridine tetraphosphate) which all demonstrated efficacy in the mouse model of infection with mouse-adapted Ebola virus (EBOV) model of disease and had similar in vitro inhibition of an Ebola pseudovirus (VSV-EBOV-GP), suggesting they interfere with viral entry. Using a machine learning model to predict lysosomotropism these compounds were evaluated for their ability to possess a lysosomotropic mechanism in vitro. We now demonstrate in vitro that pyronaridine tetraphosphate is an inhibitor of Lysotracker accumulation in lysosomes (IC50 = 0.56 μM). Further, we evaluated antiviral synergy between pyronaridine and artesunate (Pyramax®), which are used in combination to treat malaria. Artesunate was not found to have lysosomotropic activity in vitro and the combination effect on EBOV inhibition was shown to be additive. Pyramax® may represent a unique example of the repurposing of a combination product for another disease.
我们最近发现了三种分子(替洛隆、氯喹和吡咯烷四磷酸盐),它们在感染适应小鼠的埃博拉病毒(EBOV)的小鼠模型中均显示出疗效,并且对埃博拉假病毒(VSV-EBOV-GP)具有相似的体外抑制作用,表明它们干扰病毒进入。使用机器学习模型预测溶酶体趋向性,评估这些化合物在体外是否具有溶酶体趋向性机制。我们现在证明,吡咯烷四磷酸盐是溶酶体蓄积的溶酶体抑制剂(IC50=0.56μM)。此外,我们评估了吡咯烷和青蒿琥酯(Pyramax®)之间的抗病毒协同作用,这两种药物联合用于治疗疟疾。青蒿琥酯在体外没有溶酶体趋向性活性,并且对 EBOV 抑制的联合作用显示为相加作用。Pyramax®可能代表了重新利用组合产品治疗另一种疾病的独特范例。